Literature DB >> 16005222

Benzazoles as allosteric potentiators of metabotropic glutamate receptor 2 (mGluR2): efficacy in an animal model for schizophrenia.

Steven P Govek1, Celine Bonnefous, John H Hutchinson, Theodore Kamenecka, Jeffrey McQuiston, Richard Pracitto, Lucy X Zhao, Michael F Gardner, Joyce K James, Lorrie P Daggett, Blake A Rowe, Hervé Schaffhauser, Linda J Bristow, Una C Campbell, Dana E Rodriguez, Jean-Michel Vernier.   

Abstract

Metabotropic glutamate receptor 2 (mGluR2) has been implicated in a variety of CNS disorders, including schizophrenia. Disclosed herein is the development of a new series of allosteric potentiators of mGluR2. Structure-activity relationship studies in conjunction with pharmacokinetic data led to the discovery of indole 5, which is active in an animal model for schizophrenia.

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Year:  2005        PMID： 16005222     DOI： 10.1016/j.bmcl.2005.06.017

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  19 in total

Review 1.  Recent progress in the synthesis and characterization of group II metabotropic glutamate receptor allosteric modulators.

Authors:  Douglas J Sheffler; Anthony B Pinkerton; Russell Dahl; Athina Markou; Nicholas D P Cosford
Journal:  ACS Chem Neurosci       Date:  2011-04-12       Impact factor: 4.418

Review 2.  Positive allosteric modulators to peptide GPCRs: a promising class of drugs.

Authors:  Tamas Bartfai; Ming-wei Wang
Journal:  Acta Pharmacol Sin       Date:  2013-04-29       Impact factor: 6.150

Review 3.  Metabotropic glutamate receptors as therapeutic targets for schizophrenia.

Authors:  Paige N Vinson; P Jeffrey Conn
Journal:  Neuropharmacology       Date:  2011-05-19       Impact factor: 5.250

Review 4.  Allosteric modulation of metabotropic glutamate receptors.

Authors:  Douglas J Sheffler; Karen J Gregory; Jerri M Rook; P Jeffrey Conn
Journal:  Adv Pharmacol       Date:  2011

5.  Design and synthesis of an orally active metabotropic glutamate receptor subtype-2 (mGluR2) positive allosteric modulator (PAM) that decreases cocaine self-administration in rats.

Authors:  Raveendra-Panickar Dhanya; Shyama Sidique; Douglas J Sheffler; Hilary Highfield Nickols; Ananda Herath; Li Yang; Russell Dahl; Robert Ardecky; Svetlana Semenova; Athina Markou; P Jeffrey Conn; Nicholas D P Cosford
Journal:  J Med Chem       Date:  2010-12-14       Impact factor: 7.446

6.  The mGluR2 positive allosteric modulator BINA decreases cocaine self-administration and cue-induced cocaine-seeking and counteracts cocaine-induced enhancement of brain reward function in rats.

Authors:  Xinchun Jin; Svetlana Semenova; Li Yang; Robert Ardecky; Douglas J Sheffler; Russell Dahl; P Jeffrey Conn; Nicholas D P Cosford; Athina Markou
Journal:  Neuropsychopharmacology       Date:  2010-06-16       Impact factor: 7.853

Review 7.  Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia.

Authors:  P Jeffrey Conn; Craig W Lindsley; Carrie K Jones
Journal:  Trends Pharmacol Sci       Date:  2008-12-06       Impact factor: 14.819

Review 8.  Emerging approaches for treatment of schizophrenia: modulation of glutamatergic signaling.

Authors:  Meredith J Noetzel; Carrie K Jones; P Jeffrey Conn
Journal:  Discov Med       Date:  2012-11       Impact factor: 2.970

Review 9.  Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders.

Authors:  P Jeffrey Conn; Arthur Christopoulos; Craig W Lindsley
Journal:  Nat Rev Drug Discov       Date:  2009-01       Impact factor: 84.694

10.  Allosteric modulators for mGlu receptors.

Authors:  F Gasparini; W Spooren
Journal:  Curr Neuropharmacol       Date:  2007-09       Impact factor: 7.363
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